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Current Medicinal Chemistry


ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

Synthesis and Preliminary Screening of Novel Tryptamines as 5-HT4 Receptor Ligands

Author(s): A. Hanna-Elias, D.T. Manallack, I. Berque-Bestel, H.R. Irving, I.M. Coupar and M.N. Iskander

Volume 17 , Issue 25 , 2010

Page: [2775 - 2787] Pages: 13

DOI: 10.2174/092986710791859351

Price: $65


For the development of novel 5-HT4 receptor ligands we have designed and synthesized two series of 5- methoxytryptamine derivatives varying the substitution on the primary amine. Their biological activities were evaluated in a receptor binding assay where a subset of compounds showed comparable potency to the agonists serotonin and 5- methoxytryptamine. Structure-activity analyses have highlighted promising avenues for further synthetic work and binding modes were proposed by docking these compounds into a homology model of the 5-HT4 receptor.

Keywords: 5-HT4 ligands, serotonin, tryptamine, 5-HT4 receptor, medicinal chemistry

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